- |||||||||| Oclaiz (octreotide subcutaneous depot) / Camurus, Signifor (pasireotide) / Recordati, paltusotine (CRN00808) / Crinetics
Review, Journal: The current status of somatostatin analogs in the treatment of neuroendocrine tumors and future perspectives. (Pubmed Central) - Feb 1, 2025
Octreotide and lanreotide appear to be clinically interchangeable, and no signs of superiority of one agent over the other has been observed so far. Whether SSAs may be exploited in the maintenance setting following more aggressive treatments, whether continuing SSAs beyond-progression after first-line therapy could be an effective treatment strategy, and whether new-generation SSAs such as pasireotide could overcome resistance to established SSAs are key areas of investigation.
- |||||||||| Sanvar (vapreotide) / PharmGKB, Debiopharm, Bausch Health, Eisai, Germanin (suramin) / Optimum Therap, Signifor (pasireotide) / Recordati
Preclinical, Journal: Investigation into in silico and in vitro approaches for inhibitors targeting MCM10 in Leishmania donovani: a comprehensive study. (Pubmed Central) - Feb 1, 2025
In vitro experiments also demonstrated a dose-dependent reduction in L. donovani viability for suramin, vapreotide, and pasireotide, with computed IC50 values providing quantitative metrics of their anti-leishmanial efficacy. The research offers a comprehensive understanding of LdMcm10 as a drug target and provides a foundation for further investigations and clinical exploration, ultimately advancing drug discovery strategies for leishmaniasis treatment.
- |||||||||| Signifor (pasireotide) / Recordati
Enrollment open, Trial initiation date: PAMSARC: Pasireotide as Maintenance Treatment in Synovial Sarcoma and Desmoplastic Small Round Cell Tumor (clinicaltrials.gov) - Jan 13, 2025
P2, N=28, Recruiting,
The research offers a comprehensive understanding of LdMcm10 as a drug target and provides a foundation for further investigations and clinical exploration, ultimately advancing drug discovery strategies for leishmaniasis treatment. Not yet recruiting --> Recruiting | Initiation date: Sep 2024 --> Dec 2024
- |||||||||| Review, Journal: Advances in pharmacological treatment of Cushing's disease. (Pubmed Central) - Jan 12, 2025
Research on pharmacological treatments for Cushing's disease is ongoing, with new drugs such as seliciclib, CRN04894, fimepinostat, vorinostat, and SPI-62 currently in phase II clinical trial. The development of novel drugs holds promise for more precise and effective treatment for Cushing's disease patients.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Structure and Function of Somatostatin and its Receptors in Endocrinology. (Pubmed Central) - Jan 10, 2025
Somatostatin analogs, such as octreotide, lanreotide, and pasireotide, which function as somatostatin receptor ligands (SRLs), are the main drugs used for the treatment of acromegaly...The results revealed the residues that contribute to the ligand binding pocket and demonstrated that Trp8-Lys9 (the W-K motif) in somatostatin analogs is the key motif in stabilizing the bottom part of the binding pocket. In this review, we discuss the recent findings related to the structural analysis of SSTRs and SRLs, the relationships between the structural data and clinical findings, and the future development of novel structure-based therapies.
- |||||||||| Somavert (pegvisomant) / Pfizer, Signifor (pasireotide) / Recordati
Review, Journal: Novel approach to bone comorbidity in resistant acromegaly. (Pubmed Central) - Dec 10, 2024
Nonetheless, some potential protective effects may derive from vitamin D supplementation and pasireotide therapies, independently from disease status. Aim of this manuscript is to review the current and emerging evidence on skeletal fragility in patients with active and resistant acromegaly.
- |||||||||| Journal: New Trends in Treating Cushing's Disease. (Pubmed Central) - Nov 15, 2024
Levoketoconazole and osilodrostat are novel steroid inhibitors, and relacorilant overcomes the adverse effects of mifepristone. Adrenal ACTH receptor blockage and immunotherapy could also play a role.
- |||||||||| Somavert (pegvisomant) / Pfizer, Signifor (pasireotide) / Recordati
Cost-Utility of Acromegaly Second Line Pharmacological Treatments in Adult Patients in France () - Nov 4, 2024 - Abstract #ISPOREU2024ISPOR_EU_2451;
The updated model aims to offer a more thorough and comprehensive view of the cost-utility of second-line pharmacological treatments in acromegaly. Beyond clinical data, this analysis broadens our perspective within a framework where costs of treatments are rising, and healthcare system financing is more challenging.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Structural insights into somatostatin receptor 5 bound with cyclic peptides. (Pubmed Central) - Oct 19, 2024
Two cyclic SST analog peptides (pasireotide and octreotide) both can activate SSTR5 and SSTR2...Moreover, we find that the Q2.63, N6.55, F7.35 and ECL2 of SSTR2 play a crucial role in octreotide biased binding of SSTR2. Our results will provide structural insights and offer new opportunities for the drug discovery of better selective pharmaceuticals targeting specific SSTR subtypes.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Pituitary gigantism due to a novel AIP germline splice-site variant. (Pubmed Central) - Oct 11, 2024
IGF-I concentrations decreased but did not normalize. We discovered a novel germline single nucleotide variant in the splicing donor region of intron 2 of the AIP gene (NM_003977.4:c.279+1 G>A), classified as likely pathogenic according to the American College of Medical Genetics and Genomics guidelines.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Difficulties of treating acromegaly in the light of 12 years of experience (Pubmed Central) - Oct 6, 2024
We discovered a novel germline single nucleotide variant in the splicing donor region of intron 2 of the AIP gene (NM_003977.4:c.279+1 G>A), classified as likely pathogenic according to the American College of Medical Genetics and Genomics guidelines. No abstract available
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Selective ligand recognition and activation of somatostatin receptors SSTR1 and SSTR3. (Pubmed Central) - Oct 3, 2024
Here, we report four cryoelectron microscopy structures of Gi-coupled SSTR1 and SSTR3 activated by distinct agonists, including the FDA-approved panagonist pasireotide as well as their selective small molecule agonists L-797591 and L-796778...Together with mutagenesis analyses, our structures further reveal the dynamic feature of ligand binding pockets in SSTR1 and SSTR3 to accommodate divergent agonists, the key determinants of ligand selectivity lying across the orthosteric pocket of different SSTR subtypes, as well as the molecular mechanism underlying diversity and conservation of receptor activation. Our work provides a framework for rational design of subtype-selective SSTR ligands and may facilitate drug development efforts targeting SSTRs with improved therapeutic efficacy and reduced side effects.
- |||||||||| Signifor (pasireotide) / Recordati
Journal, Metastases: Genomic and transcriptomic features of androgen receptor signaling inhibitor resistance in metastatic castration-resistant prostate cancer. (Pubmed Central) - Oct 1, 2024
We found that patients with SSTR1-low mCRPC tumors derived less benefit from subsequent ARSI therapy in a retrospective cohort. We showed that SSTR1 was antiproliferative in 22Rv1 cells and that the FDA-approved drug pasireotide suppressed 22Rv1 cell proliferation.CONCLUSIONOur findings expand the knowledge of ARSI resistance and point out actionable next steps, exemplified by potentially targeting SSTR1, to improve patient outcomes.FUNDINGNational Cancer Institute (NCI), NIH; Prostate Cancer Foundation; Conquer Cancer, American Society of Clinical Oncology Foundation; UCSF Benioff Initiative for Prostate Cancer Research; Netherlands Cancer Institute.
- |||||||||| Somavert (pegvisomant) / Pfizer, Signifor (pasireotide) / Recordati, Signifor LAR (pasireotide long acting release) / Recordati
Retrospective data, Journal: GH receptor polymorphisms guide second-line therapies to prevent acromegaly skeletal fragility: preliminary results of a pilot study. (Pubmed Central) - Sep 20, 2024
Our data support a predictive role of the GHR isoforms for the occurrence of i-VFs in acromegalic patients treated with second-line drugs, tailored to the individual patient. The knowledge of the GHR polymorphism may facilitate the choice of second-line therapies, improving the therapeutic approach, in the context of personalized medicine.
- |||||||||| Signifor (pasireotide) / Recordati
Successful Management of Pancreatic Insulinoma by Endoscopic Ultrasound Guided Radio Frequency Ablation (Exhibit Hall E) - Aug 20, 2024 - Abstract #ACG2024ACG_5009;
Patient was treated with off-label Pasireotide/diazoxide for glycemic control...This case provides an example of the expanding role for EUS RFA to treat pancreatic insulinomas, and should encourage expansion of inclusion criteria for any pending head-to-head trials of EUS RFA vs surgical resection. Figure: A 23mm x 16mm Insulinoma seen on EUS.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Rapid Resolution of Recalcitrant Headache With Pasireotide in an Adult Patient With Acromegaly. (Pubmed Central) - Aug 12, 2024
Following a switch to pasireotide, the patient reported rapid and complete resolution of headaches and normalization of IGF-1 levels within a month of the treatment switch. This report underscores the challenges in acromegaly management and confirms the potential utility of pasireotide for patients suffering from treatment-resistant headache.
- |||||||||| Signifor (pasireotide) / Recordati
Review, Journal: Predictors of biochemical response to somatostatin receptor ligands in acromegaly. (Pubmed Central) - Jul 21, 2024
The potential solution to the limitations of traditional methods involves combining systems biology with artificial intelligence, which is currently providing answers to such long-standing questions that may eventually be finally included into the clinical guidelines and make personalized medicine a reality. The aim of this review is to describe the current knowledge of the main fg-SRLs and pasireotide response predictors, discuss their current usefulness, and point to future directions in the research of this field.
- |||||||||| Signifor (pasireotide) / Recordati
Review, Journal: Current role of pasireotide in the treatment of acromegaly. (Pubmed Central) - Jul 21, 2024
Here we elucidate the molecular pathways of resistance to first-generation SSTRA, the mechanism of action, pre-clinical and clinical evidence of the use of pasireotide in patients having incomplete / lack of response to first-generation SSTRA. We also discuss the clinical, pathological, and radiological markers predicting response to pasireotide, and the difference in side-effect profiles of pasireotide, compared to first-generation SSTRA.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Case report: Exceptional transmission of congenital hyperinsulinism from a focal CHI mother to her diffuse CHI dichorionic diamniotic twins. (Pubmed Central) - Jul 2, 2024
Due to the recurrence of hypoglycaemia episodes despite reaching maximum doses of Octreotide, from day 92 the treatment was switched to Pasireotide...This case emphasises the significance of genetic counselling for individuals with a history of rare diseases outside the context of consanguinity, as there is a potential risk of recurrence. Prenatal diagnosis can lead to better outcomes for affected neonates, as well as help families make informed decisions about future pregnancies.
- |||||||||| Somavert (pegvisomant) / Pfizer, Signifor (pasireotide) / Recordati
Journal: Acromegaly management in the Nordic countries: (Pubmed Central) - Jun 12, 2024
Prenatal diagnosis can lead to better outcomes for affected neonates, as well as help families make informed decisions about future pregnancies. This consensus exploration study on the management of patients with acromegaly in the Nordic countries revealed a relatively large degree of disagreement among experts, which mirrors the complexity of the disease and the shortage of evidence-based data.
- |||||||||| Somavert (pegvisomant) / Pfizer, Signifor (pasireotide) / Recordati
Journal: Standards of care for medical management of acromegaly in pituitary tumor centers of excellence (PTCOE). (Pubmed Central) - Jun 4, 2024
Moreover, at odds with consensus guidelines, other monotherapies for acromegaly appear to have a marginal role as compared to combination therapies as extrapolated from PTCOE practice data. Presence of uncontrolled patients in each treatment category suggest that further optimization of medical therapy, as well as use of other therapeutic tools such as radiosurgery may be needed.
- |||||||||| Somavert (pegvisomant) / Pfizer, Signifor (pasireotide) / Recordati
Retrospective data, Journal: Pegvisomant or pasirotide in PRL and GH co-secreting vs GH-secreting Pit-NETs. (Pubmed Central) - May 28, 2024
Active, not recruiting --> Completed Despite the more aggressive behavior of GH/PRL-Pit-NETs than GH-Pit-NETs, no differences in the rate of IGF-1 control with pegvisomant and pasireotide is observed between both groups, and both drugs are effective treatments to control IGF-1 and PRL hypersecretion in these tumors.
- |||||||||| Signifor (pasireotide) / Recordati
Pasireotide in Acromegaly: long-term efficacy and safety (Exhibition Area) - Mar 17, 2024 - Abstract #ICEEDEC2024ICE_EDEC_681;
Older patients and higher IGF-I, glucose and HbA1c at baseline were associated with higher glucose and HbA1c during pasireotide therapy. In conclusion, sustained biochemical control and manageable side effects were observed during more than 11 years of treatment with pasireotide in patients with acromegaly.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Management of pasireotide-induced hyperglycemia in patients with acromegaly: An experts' consensus statement. (Pubmed Central) - Mar 1, 2024
Our expert recommendations address the specific pathophysiology of pasireotide-induced hyperglycemia by recommending the incretin-based therapeutics dipeptidyl peptidase-4 inhibitors (DPP-4i) and glucagon-like peptide-1 receptor agonists (GLP-1 RA) in all appropriate patients as an alternative to first-line monotherapy with metformin. Furthermore, we emphasize the importance of adequate control of acromegaly, excellent diabetes education, nutrition and lifestyle guidance and advise to consult expert diabetologists in case of uncertainty in the management of patients with hyperglycemia under pasireotide.
- |||||||||| Signifor (pasireotide) / Recordati, Signifor LAR (pasireotide long acting release) / Recordati, pasireotide long-acting depot (CAM4071) / Camurus
PK/PD data, Journal: Pharmacokinetics and pharmacodynamics of a pasireotide subcutaneous depot (CAM4071) and comparison with immediate and long-acting release pasireotide. (Pubmed Central) - Feb 29, 2024
Furthermore, we emphasize the importance of adequate control of acromegaly, excellent diabetes education, nutrition and lifestyle guidance and advise to consult expert diabetologists in case of uncertainty in the management of patients with hyperglycemia under pasireotide. CAM4071 provided long-acting release of pasireotide over at least one month, with high bioavailability and onset and duration of IGF-1 suppression similar to pasireotide LAR.
- |||||||||| Signifor (pasireotide) / Recordati, Signifor LAR (pasireotide long acting release) / Recordati
Journal, Real-world evidence, Real-world: Efficacy of pasireotide LAR for acromegaly: a prolonged real-world monocentric study. (Pubmed Central) - Feb 20, 2024
Tumor shrinkage was observed in 6 out of 7 evaluated responders, with no cases of size increase during the long-term follow-up. Pas-LAR is effective and safe and the early identification of responders is possible just after the first administration.
- |||||||||| Somavert (pegvisomant) / Pfizer, Signifor (pasireotide) / Recordati
Biomarker, Review, Journal: Biomarkers of response to treatment in acromegaly. (Pubmed Central) - Jan 3, 2024
Biomarkers for fg-SRL that can already be applied in clinical practice are: gender, age, pretreatment GH and IGF-I levels, cytokeratin granulation pattern, and the expression of somatostatin receptor type 2. Using biomarkers of response could guide treatment towards precision medicine with greater efficacy and lower costs.
- |||||||||| Signifor (pasireotide) / Recordati
Journal: Pasireotide - potential treatment option for McCune Albright-associated acromegaly. (Pubmed Central) - Dec 21, 2023
All three patients developed intermittent impaired fasting glucose, without the need for glucose-lowering drugs. Thus, pasireotide LAR is clearly useful as third-line therapy, and potentially even as second-line therapy, in MAS-associated acromegaly.
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